Patents Assigned to Merck & Co.
  • Patent number: 4397851
    Abstract: Antimicrobial compounds of the formula: ##STR1## wherein Hal is bromine or chlorine; R is C.sub.1-4 alkyl, straight or branched chain; and one of R.sup.1 and R.sup.2 is hydrogen and the other is selected from the group consisting of C.sub.3-8 cycloalkyl; C.sub.3-8 cycloalkyl C.sub.1-3 alkyl; phenyl; phenyl C.sub.1-3 alkyl; mono- or disubstituted phenyl or phenyl C.sub.1-3 alkyl wherein the substituents are halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, hydroxy, nitro, cyano, or trifluoromethyl; a heterocyclic radical selected from the group consisting of thienyl, furanyl, pyrrolyl, isoxazolyl, oxazolyl, isothiazolyl, thiazolyl, pyrazolyl, imidazolyl, pyridazinyl, pyrimidinyl, pyrazinyl, and pyridinyl, and N-oxides thereof; and a saturated heterocyclic radical selected from the group consisting of pyrrolidinyl, tetrahydrofuranyl, tetrahydrothienyl, isoxazolidinyl, oxazolidinyl, isothiazolidinyl, thiazolidinyl, pyrazolidinyl, imidazolidinyl, piperazinyl, and piperidinyl.
    Type: Grant
    Filed: December 22, 1981
    Date of Patent: August 9, 1983
    Assignee: Merck & Co., Inc.
    Inventors: John E. Engelhart, Marshall R. Angeles, Michael J. D'Errico
  • Patent number: 4397786
    Abstract: Statine (Sta), a naturally-occurring amino acid and closely related derivatives, are prepared by a novel method involving an oxidative route to the requisite chiral .alpha.-aminoaldehyde intermediate, L-leucinal; the novel method may be illustrated by the following reaction scheme: ##STR1## .
    Type: Grant
    Filed: November 23, 1981
    Date of Patent: August 9, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Ben E. Evans, Kenneth E. Rittle
  • Patent number: 4396616
    Abstract: Substituted enantholactam dipeptides and derivatives thereof are disclosed which are useful as converting enzyme inhibitors and as antihypertensives.
    Type: Grant
    Filed: September 4, 1981
    Date of Patent: August 2, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Elbert E. Harris, David Taub, Eugene D. Thorsett
  • Patent number: 4394385
    Abstract: The invention relates to the treatment of gray matter edema in the brain or spinal chord by the administration of benzofuranyloxyacetic acids, indeno[5,4-b]furancarboxylic acids, their analogs and salts thereof.
    Type: Grant
    Filed: January 29, 1982
    Date of Patent: July 19, 1983
    Assignee: Merck & Co., Inc.
    Inventor: Edward J. Cragoe, Jr.
  • Patent number: 4394515
    Abstract: Novel 7- and 8-R-10,11-dihydro-11-oxodibenzo[b,f]thiepin derivatives are employed in the treatment and control of allergic conditions such as allergic asthma.
    Type: Grant
    Filed: April 6, 1981
    Date of Patent: July 19, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Joshua Rokach, Clarence S. Rooney, Edward J. Cragoe, Jr.
  • Patent number: 4393242
    Abstract: Methylvanillyl ketone is prepared from a "through process" involving oxidation of isoeugenol followed by subsequent acidic hydrolysis.
    Type: Grant
    Filed: July 6, 1981
    Date of Patent: July 12, 1983
    Assignee: Merck & Co., Inc.
    Inventor: Meyer Sletzinger
  • Patent number: 4393046
    Abstract: Combinations of thiopeptin or one of its analogs with a pyromellitic diimide are shown to synergistically increase the feed efficiency of economically important ruminant animals, especially cattle, sheep, and goats.
    Type: Grant
    Filed: January 30, 1981
    Date of Patent: July 12, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Francis P. Baylis, Gary E. Smith
  • Patent number: 4393212
    Abstract: Novel substituted (3-loweralkylamino-2-R.sub.1 O-propoxy)pyridines, their pharmaceutically acceptable salts, certain intermediates and their preparation are disclosed. These pyridines have pharmaceutically useful properties such as .beta.-adrenergic blocking activity.
    Type: Grant
    Filed: May 13, 1981
    Date of Patent: July 12, 1983
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Gerald S. Ponticello
  • Patent number: 4391800
    Abstract: 2-Amino-2-deoxy-.beta.-D-glucopyranosyl-(1-4)-2-amino-2-deoxy-D-glucoses of the general structural formula: ##STR1## wherein R.sub.1 is hydrogen, alkyl (1-7C), substituted alkyl (1-7C), phenyl, substituted phenyl, benzyl, or substituted benzyl;R.sub.2 is alkyl, substituted alky, phenyl, or substituted phenyl and each R.sub.2 may be the same group or a different group;R.sub.3 is H or ##STR2## wherein R.sub.8 is H or lower alkyl (1-10C), and provided at least one of R.sub.3 is not H,R.sub.9 is H, or R.sub.9 -R.sub.10 together is --CH.sub.2 --CH.sub.2 --CH.sub.2 --;R.sub.10 is H, alkyl (L-7C), hydroxymethyl, mercaptomethyl, benzyl, or substituted benzyl;R.sub.11 and R.sub.12 each is carboxyl, esterified carboxyl (1-7C), amidated carboxyl, or mono- or di-alkyl- (1-3C) amidated carboxyl;R.sub.4 and R.sub.5 are the same or different and are H, aliphatic or aromatic acyl (2-21C) or substituted acyl (2-21C);when R.sub.8 is lower alkyl, the stereochemistry at asymmetric center I can be either D or L;when R.sub.
    Type: Grant
    Filed: April 27, 1979
    Date of Patent: July 5, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Philippe L. Durette, Tsung-Ying Shen
  • Patent number: 4391812
    Abstract: Antimicrobial agents suitable for use in aqueous systems for their preservation against biodeterioration include substitutedpiperidinomethylpropenenitriles and propanenitriles. The unsaturated compounds are prepared by reaction of a suitable piperidine with cyano acetic acid and formaldehyde: the propane derivatives therefrom by nucleophilic addition.
    Type: Grant
    Filed: March 24, 1982
    Date of Patent: July 5, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Richard A. Dybas, Nathaniel Grier, Bruce E. Witzel
  • Patent number: 4390546
    Abstract: There is disclosed a macrolide isolated from the fermentation broth of a microorganism identified as MA-5285 which morphological analysis reveals to be a strain of Streptomyces hygroscopicus. The compound's structure is presented based upon analytical studies. The compound has insecticidal and antiparasitic activity.
    Type: Grant
    Filed: December 7, 1981
    Date of Patent: June 28, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Michael A. Goetz, Pamela A. McCormick, Richard L. Monaghan
  • Patent number: 4390693
    Abstract: Novel cephalosporin compounds having a substituted or unsubstituted vinyl group at the 3-position are prepared by the reaction of a phosphoranylidene compound with a compound containing a carbonyl group. The novel cephalosporin compounds are active against a range of gram-negative and gram-positive microorganisms and are of value in human and veterinary medicine.
    Type: Grant
    Filed: October 9, 1980
    Date of Patent: June 28, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Thomas R. Beattie, John Hannah, David B. R. Johnston
  • Patent number: 4390537
    Abstract: 1-(Substituted-aminoalkoxyphenyl)-2-methylene-1-alkanones, a class of compounds possessing anti-allergic properties for use in the treatment of allergic conditions, such as asthma prepared by etherifying an alkanoylphenol with an aminoalkyl halide, converting the ether formed to a salt of Mannich base by reacting it with a salt of a secondary amine in the presence of formaldehyde or paraformaldehyde and treating the Mannich salt with a weak base to deaminate the same and form the final product.
    Type: Grant
    Filed: May 19, 1982
    Date of Patent: June 28, 1983
    Assignee: Merck & Co., Inc.
    Inventor: Edward J. Cragoe, Jr.
  • Patent number: 4390703
    Abstract: Some derivatives of interphenylene-9-thia-11-oxo-12-azaprostanoic acid which are active renal vasodilator agents are resolved via diastereomeric camphanyl or camphorcarbonyl esters. Upon hydrolysis, the separated diastereoisomers yield optically pure enantiomers.
    Type: Grant
    Filed: June 22, 1981
    Date of Patent: June 28, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Mark G. Bock, Robert M. Di Pardo
  • Patent number: 4389417
    Abstract: The invention relates to the treatment of gray matter edema in the brain or spinal chord by the administration of (indanyloxy)acetic acids, and analogs and salts thereof.
    Type: Grant
    Filed: December 30, 1981
    Date of Patent: June 21, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Robert S. Bourke, Edward J. Cragoe, Jr.
  • Patent number: 4389525
    Abstract: A process for resolving certain interphenylene-9-thia-11-oxo-12-azaprostanoic acids using camphanic or a camphor carboxylic acid, certain intermediates and optically pure azaprostanoic acids are disclosed.
    Type: Grant
    Filed: June 22, 1981
    Date of Patent: June 21, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Mark G. Bock, Robert M. Di Pardo
  • Patent number: 4389397
    Abstract: Ivermectin, an antiparasitic agent which is insoluble and unstable in water, is solubilized by the formation of colloidal particles, called micelles, with surface active agents as solubilizers and stabilized by using cosolvents and/or appropriate substrates in the aqueous formulation. The liquid formulations are suitable for use as parenteral or oral administration for the treatment of parasitic infections.
    Type: Grant
    Filed: September 21, 1981
    Date of Patent: June 21, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Pak-Kan A. Lo, James B. Williams
  • Patent number: 4389415
    Abstract: A pharmaceutical composition containing .alpha.-methyl-p-tyrosine and carbidopa and method of treating hypertension are described.
    Type: Grant
    Filed: July 20, 1981
    Date of Patent: June 21, 1983
    Assignee: Merck & Co., Inc.
    Inventor: Alexander Scriabine
  • Patent number: 4388475
    Abstract: Organic sulfoxides having a latent allyl group bound to the sulfur are enzyme inhibitors of the suicide or K.sub.cat type.
    Type: Grant
    Filed: May 7, 1980
    Date of Patent: June 14, 1983
    Assignee: Merck & Co., Inc.
    Inventor: Raymond A. Firestone
  • Patent number: 4388310
    Abstract: Disclosed are 6-amido-2-S-oxides of substituted 2-organothio-pen-2-em-3-carboxylic acids (I) which are useful as antibiotics and as intermediates in the synthesis of substituted pen-2-em-3-carboxylic acids: ##STR1## wherein: R.sup.1 is H or acyl; R.sup.2 is hydrogen or methoxyl; R.sup.3 is alkyl having from 1-6 carbon atoms; phenylalkyl having 7-12 carbon atoms; and cycloalkyl having 3-6 carbon atoms; and R.sup.4 is hydrogen, a removable protecting group or a pharmaceutically acceptable salt or ester moiety.
    Type: Grant
    Filed: March 1, 1982
    Date of Patent: June 14, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Burton G. Christensen, Frank P. DiNinno, David A. Muthard, Ronald W. Ratcliffe